Pentosan polysulfate

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Pentosan polysulfate
Clinical data
AHFS/Drugs.comConsumer Drug Information
Pregnancy cat.B
Legal status ?
RoutesOral, intramuscular, intra-articular, intraventricular
Pharmacokinetic data
ExcretionUrine
Identifiers
CAS number37300-21-3 YesY (free acid)
116001-96-8 (sodium salt)
ATC codeC05BA04 G04BX15 QM01AX90
PubChemCID 37720
Chemical data
Formula(C5H6Na2O10S2)n
 YesY (what is this?)  (verify)
 
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Pentosan polysulfate
Clinical data
AHFS/Drugs.comConsumer Drug Information
Pregnancy cat.B
Legal status ?
RoutesOral, intramuscular, intra-articular, intraventricular
Pharmacokinetic data
ExcretionUrine
Identifiers
CAS number37300-21-3 YesY (free acid)
116001-96-8 (sodium salt)
ATC codeC05BA04 G04BX15 QM01AX90
PubChemCID 37720
Chemical data
Formula(C5H6Na2O10S2)n
 YesY (what is this?)  (verify)

Pentosan polysulfate sold under the name Elmiron by Ortho-McNeil Pharmaceutical and "Comfora" by Swati Spentose Pvt. Ltd. in India is the only oral medication approved by the U.S. Food and Drug Administration (FDA) for the treatment of interstitial cystitis (IC), also known as painful bladder syndrome.

Contents

Uses

Interstitial cystitis/painful bladder syndrome

Interstitial cystitis/painful bladder syndrome (IC/PBS) patients struggle with symptoms of urinary frequency, urgency, pressure and/or pain, as well as nocturia (frequent urination at night), dyspareunia (painful intercourse), pain and/or discomfort while sitting in a car, while driving and/or travelling.

The origin/cause of IC/PBS is currently unknown though a number of theories are currently under consideration. Urine cultures are typically negative for infection, yet it is not unusual for patients to believe that they have had infections for years rather than IC/PBS, because the symptoms of IC/PBS mimic those of an infection.

Pentosan polysulfate is available as pills or as a direct infusion into the bladder.

Transmissible spongiform encephalopathies

Recently pentosan polysulfate has gained attention as possibly being effective in the treatment of Creutzfeldt-Jakob disease (CJD), although there is currently no definitive evidence for this idea other than results of the ongoing treatment (published) of one patient in Northern Ireland and around six other patients in mainland Britain.[1]

Around 15 other patients in non-UK countries have also received this treatment in an attempt to halt or slow down CJD and related disease progression.

Osteoarthrosis in adult dogs

Recently PPN is being marketed as an alternative for the treatment of lameness and pain of degenerative joint disease/osteoarthrosis (non-infectious arthrosis) in the skeletally mature dog.

Cartrophen-Vet is a 100mg/ml formulation of Pentosan polysulphate that has been used in Australia since the early 1990s. It is produced by Biopharm Australia.[2]

3 mg/kg PPN is given subcutaneously every 5-7 days for 4 treatments. Subsequent single booster shots are usually given every 3-6 months.[3]

Pharmacology

Pentosan is 1/15 Heparin. Heparin is an anticoagulant.

Pentosan is believed to work by providing a protective coating to the damaged bladder wall. However, Pentosan has exceptionally poor bioavailability when taken orally. Research presented in 2005 by Alza Pharmaceuticals demonstrates that more than 94% of the medication is excreted, intact, in feces without providing any beneficial effect.[4] Their research found that only 6% was excreted through urine. The drug must be taken for several months for most patients to achieve some benefit.

More recently, pentosan polysulfate has been studied as part of a "rescue instillation" which is placed directly in the bladder and can, perhaps, provide better effectiveness. Research presented in 2005 showed a 90% effectiveness in reducing the symptoms of IC/PBS patients by using this instillation.[5]

Dosage

IC patients take one 100mg Elmiron three times a day on an empty stomach with a full glass of water.[6]

Side effects

Patients who have taken pentosan orally report a variety of side effects, primarily gastrointestinal complaints such as diarrhea, heartburn, and stomach pain.[6] Hair loss, headache, rash, and insomnia have also been reported.[6] Due to Elmiron's anticoagulant effects, some patients report bruising more easily. In some cases, patients are asked to stop taking the medication before any major surgical procedures to reduce the likelihood of bleeding.

References

  1. ^ BBC NEWS | Health | Research will now assess CJD drug
  2. ^ http://www.cartrophen.com/
  3. ^ http://www.vmd.gov.uk/espcsite/Documents/176337.DOC
  4. ^ Simon M, McClanahan RH, Shah JF et al. Metabolism of [3H]pentosan polysulfate sodium (PPS) in healthy human volunteers. Xenobiotica. 2005 Aug;35(8):775-84. PMID 16278190
  5. ^ Parsons, C (2005). "Successful downregulation of bladder sensory nerves with combination of heparin and alkalinized lidocaine in patients with interstitial cystitis". Urology 65 (1): 45–8. doi:10.1016/j.urology.2004.08.056. PMID 15667861.
  6. ^ a b c Pubmed Health (2012). "Pentosan Polysulfate". U.S. National Library of Medicine. http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000188/. Retrieved 2 October 2012.

External links